Thiazolidine are versatile heterocyclic organic compound deemed essential medically-active compounds and interesting building blocks that can be used to create biologically active derivatives, among this class and have many potential biological and pharmacological effects including anti-proliferative, anti-viral, anti-arrhythmia, anti-tubercular, anti-microbial, anti-diabetic, antifungal, antioxidant, anti-inflammatory, anticonvulsant, and anticancer. Thiazolidine (TZD) is currently often utilized in modern medicine due to its organic features. ‎TZD derivatives and their complexes were characterized using various spectroscopic approaches, including infrared, and ultraviolet-visible measurements. TZD derivatives are created when their molecular composition is modified, increasing the probability that they will bind to proteins. In the present review, we present a summary of twenty years of research and investigations on TZD synthesis approaches as well as anticancer properties of TZD derivatives and their structure activity relationship (SAR). With great therapeutic results, it has been employed to treat a wide range of disorders. Therefore, it is a promising drug with a lot of scope for study.